| Attributes | Values |
|---|
| rdf:type
| |
| http://linked.open...gbank/description
| - Iloperidone is an atypical antipsychotic for the treatment of schizophrenia symptoms. Hoechst Marion Roussel Inc. made initial inquiries into the drug; however, in May 1996, they discontinued research, and in June 1997 gave research rights to Titan Pharmaceuticals. Titan then handed over worldwide development, manufacturing and marketing rights to Novartis in August 1998. On June 9, 2004, Titan Pharmaceuticals announced that the Phase III development rights have been acquired by Vanda Pharmaceuticals. FDA approved on May 9, 2009. (en)
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| http://linked.open...y/drugbank/dosage
| |
| http://linked.open...generalReferences
| - # Strupczewski JT, Bordeau KJ, Chiang Y, Glamkowski EJ, Conway PG, Corbett R, Hartman HB, Szewczak MR, Wilmot CA, Helsley GC: 3-[[(Aryloxy)alkyl]piperidinyl]-1,2-benzisoxazoles as D2/5-HT2 antagonists with potential atypical antipsychotic activity: antipsychotic profile of iloperidone (HP 873). J Med Chem. 1995 Mar 31;38(7):1119-31. "Pubmed":http://www.ncbi.nlm.nih.gov/pubmed/7707315 # Kongsamut S, Roehr JE, Cai J, Hartman HB, Weissensee P, Kerman LL, Tang L, Sandrasagra A: Iloperidone binding to human and rat dopamine and 5-HT receptors. Eur J Pharmacol. 1996 Dec 19;317(2-3):417-23. "Pubmed":http://www.ncbi.nlm.nih.gov/pubmed/8997630 # Hesselink JM: Iloperidone (Novartis). IDrugs. 2002 Jan;5(1):84-90. "Pubmed":http://www.ncbi.nlm.nih.gov/pubmed/12861482 # Hesselink JM: Iloperidone (Hoechst Marion Roussel Inc). IDrugs. 1999 Jun;2(6):584-90. "Pubmed":http://www.ncbi.nlm.nih.gov/pubmed/16127622 # Szewczak MR, Corbett R, Rush DK, Wilmot CA, Conway PG, Strupczewski JT, Cornfeldt M: The pharmacological profile of iloperidone, a novel atypical antipsychotic agent. J Pharmacol Exp Ther. 1995 Sep;274(3):1404-13. "Pubmed":http://www.ncbi.nlm.nih.gov/pubmed/7562515 # Bobo WV: Asenapine, iloperidone and lurasidone: critical appraisal of the most recently approved pharmacotherapies for schizophrenia in adults. Expert Rev Clin Pharmacol. 2013 Jan;6(1):61-91. doi: 10.1586/ecp.12.70. "Pubmed":http://www.ncbi.nlm.nih.gov/pubmed/23272794 # Citrome L: Iloperidone: chemistry, pharmacodynamics, pharmacokinetics and metabolism, clinical efficacy, safety and tolerability, regulatory affairs, and an opinion. Expert Opin Drug Metab Toxicol. 2010 Dec;6(12):1551-64. doi: 10.1517/17425255.2010.531259. Epub 2010 Nov 1. "Pubmed":http://www.ncbi.nlm.nih.gov/pubmed/21034370 (en)
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| http://linked.open...gy/drugbank/group
| |
| http://linked.open...drugbank/halfLife
| - The observed mean elimination half-lives for iloperidone, P88 and P95 in CYP2D6 extensive metabolizers (EM) are 18, 26 and 23 hours, respectively, and in poor metabolizers (PM) are 33, 37 and 31 hours, respectively. (en)
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| http://linked.open...ugbank/indication
| - Treatment of acute schizophrenia. (en)
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| sameAs
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| Title
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| adms:identifier
| |
| http://linked.open...mechanismOfAction
| - Iloperidone is a dopamine D2 and 5-HT2A receptor antagonist and acts as a neuroleptic agent. (en)
|
| http://linked.open...y/drugbank/patent
| |
| http://linked.open...outeOfElimination
| - Renal (in which <1% of iloperidone is excreted unchanged). (en)
|
| http://linked.open.../drugbank/synonym
| - Fanapt (en)
- Fanapta (en)
- HP 873 (en)
- Iloperidona (en)
- Iloperidonum (en)
- Zomaril (en)
- 1-[4-[3-[4-(6-Fluoro-1,2-benzisoxazol-3-yl)-1- piperidinyl]propoxy]-3-methoxyphenyl]ethanone (en)
- 4'-(3-(4-(6-Fluoro-1,2-benzisoxazol-3-yl)piperidino)propoxy)-3'-methoxyacetophenone (en)
|
| http://linked.open...drugbank/toxicity
| - Commonly observed adverse reactions (incidence ≥5% and two-fold greater than placebo) were: dizziness, dry mouth, fatigue, nasal congestion, orthostatic hypotension, somnolence, tachycardia, and weight increased. (en)
|
| http://linked.open...umeOfDistribution
| - Apparent Vd = 1340-2800 L (en)
|
| http://linked.open.../drug/hasAHFSCode
| |
| http://linked.open...k/foodInteraction
| - Administration of iloperidone with a standard high-fat meal did not significantly affect the Cmax or AUC of iloperidone, P88, or P95, but delayed Tmax by 1 hour for iloperidone, 2 hours for P88 and 6 hours for P95. (en)
- Can be taken with or without meals (en)
|
| http://linked.open...nk/proteinBinding
| - 95% of iloperidone is bound to protein. Percent bound is not altered by renal or hepatic impairment or combination therapy with ketoconazole. (en)
|
| http://linked.open...ynthesisReference
| - "DrugSyn.org":http://www.drugsyn.org/Iloperidone.htm (en)
|
| foaf:page
| |
| http://linked.open...ugbank/IUPAC-Name
| |
| http://linked.open...gy/drugbank/InChI
| |
| http://linked.open...Molecular-Formula
| |
| http://linked.open.../Molecular-Weight
| |
| http://linked.open...noisotopic-Weight
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| http://linked.open...y/drugbank/SMILES
| |
| http://linked.open.../Water-Solubility
| |
| http://linked.open...ogy/drugbank/logP
| |
| http://linked.open...ogy/drugbank/logS
| |
| http://linked.open...l/drug/hasATCCode
| |
| http://linked.open...nd-Acceptor-Count
| |
| http://linked.open...-Bond-Donor-Count
| |
| http://linked.open...drugbank/InChIKey
| |
| http://linked.open...urface-Area--PSA-
| |
| http://linked.open...nk/Polarizability
| |
| http://linked.open...bank/Refractivity
| |
| http://linked.open...atable-Bond-Count
| |
| http://linked.open...ugbank/absorption
| - Well absorbed from the GI tract and Cmax is reached within 2-4 hours. Steady-state concentration is achieved in 3-4 days post-administration of iloperidone. Relative bioavailability of the tablet formulation compared to oral solution is 96%. Accumulation occurs in a predictable fashion. (en)
|
| http://linked.open.../affectedOrganism
| - Humans and other mammals (en)
|
| http://linked.open...casRegistryNumber
| |
| http://linked.open...rugbank/clearance
| - Apparent clearance (clearance/bioavilability) = 47-102 L/h. (en)
|
| http://linked.open...k/Bioavailability
| |
| http://linked.open...bank/Ghose-Filter
| |
| http://linked.open...nk/MDDR-Like-Rule
| |
| http://linked.open...k/Number-of-Rings
| |
| http://linked.open...siological-Charge
| |
| http://linked.open...bank/Rule-of-Five
| |
| http://linked.open...tional-IUPAC-Name
| |
| http://linked.open...strongest-acidic-
| |
| http://linked.open...-strongest-basic-
| |
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